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Published in Caroline Ashley, Aileen Dunleavy, John Cunningham, The Renal Drug Handbook, 2018
Caroline Ashley, Aileen Dunleavy, John Cunningham
The plasma concentrations of the N-demethylated active metabolite are only 10–20% of those of parent, so would not be expected to significantly contribute to the therapeutic action of eletriptan. Non-renal clearance accounts for approximately 90% of the total clearance indicating that eletriptan is eliminated primarily by metabolism.
Migraine: diagnosis and treatment
Published in Stephen D. Silberstein, Richard B. Upton, Peter J. Goadsby, Headache in Clinical Practice, 2018
Stephen D. Silberstein, Richard B. Upton, Peter J. Goadsby
Oral eletriptan, with a 50% bioavailability and a half-life of 5 hours, is rapidly absorbed.77 Eletriptan has interactions with drugs that are metabolized by cytochrome p450 (including C4P3A4). Eletriptan 40 mg was at least as good as sumatriptan 100 mg at 2 hours, and eletriptan 80 mg was superior to sumatriptan 100 mg in a parallel-group controlled study. Headache improvement was evident at 1 hour, with a response rate of 43% in patients who received eletriptan 40 mg and 40% in patients who received eletriptan 80 mg (currently registered in Switzerland; this dosage is not registered in the USA), compared with only 21% and 19% for those who received sumatriptan and placebo, respectively. Treatment–related adverse events were reported by 23% of patients on placebo, 18% of patients on eletriptan 20 mg, 25% of patients on eletriptan 40 mg, 36% of patients on eletriptan 80 mg, and 37% of patients on sumatriptan 100 mg.78
Migraine Medications
Published in Gary W. Jay, Clinician’s Guide to Chronic Headache and Facial Pain, 2016
The studies showed a dose-related headache response at two hours, with eletriptan 20 mg having headache response between 47% and 54%; eletriptan 40 mg having responses between 62% and 65%, and eletriptan 80 mg having responses between 59% and 77% versus placebo responses from 19% to 24% at two hours. Eletriptan 40 mg was more effective than eletriptan 20 mg and had fewer side effects than the 80-mg dose (3).
Differential pharmacokinetic drug-drug interaction potential of eletriptan between oral and subcutaneous routes
Published in Xenobiotica, 2019
Harilal Patel, Nirmal Desai, Prakash Patel, Nirav Modi, Krunal Soni, Nitin Dobaria, Nuggehally R. Srinivas
Eletriptan has been approved for the treatment of acute migraine with or without aura in adult subjects (RELPAX® Package Insert, 2018). Following oral administration in humans, eletriptan was well absorbed and peak concentrations were attained within 1–1.5 h and the plasma concentrations of eletriptan generally appeared linear across the tested oral dose ranges from 10 to 120 mg (RELPAX® Package Insert, 2018; Shah et al., 2002). The absolute oral bioavailability was reported to be ∼50% and the terminal elimination half-life values were generally 4–5 h in human volunteers (Milton et al., 2002). Since eletriptan was subject to extensive Cytochrome P450 isoenzyme CYP3A4 metabolism (Evans et al., 2003), the use of several potent CYP3A4 inhibitors such as ketoconazole, itraconazole, nefazodone, troleandomycin, clarithromycin, ritonavir etc. are contraindicated when patients are administered eletriptan (RELPAX® Package Insert, 2018).
Menstrual migraine: a review of current and developing pharmacotherapies for women
Published in Expert Opinion on Pharmacotherapy, 2018
G. Allais, Giulia Chiarle, Silvia Sinigaglia, Chiara Benedetto
Only one study to date has evaluated the use of eletriptan for short-term prophylaxis of MM [85]. Prophylaxis with eletriptan 20 mg tid for 6 days during the PMW for 3 months was administered in 126 women, 102 of which with MM. The number of MM days and headache activity (number of attacks and severity) were lower in the phase before and after treatment in both the group with a diagnosis of certain migraine (p = 0.008) and in that with a diagnosis of probable migraine (p = 0.003), whereas no change in NMM episodes was noted. However, among those subjects who remained headache-free during the 6 days of eletriptan treatment, migraines occurred in 9% of cases during the 3 days immediately after discontinuing eletriptan therapy.
Prolonged coma resulting from massive levothyroxine overdose and the utility of N-terminal prohormone brain natriuretic peptide (NT-proBNP)
Published in Clinical Toxicology, 2019
Ophelia Wong, Anselm Wong, Shaun Greene, Andis Graudins
Coma and thyrotoxic signs are described in adults after repeated supratherapeutic ingestion of levothyroxine. Prolonged coma in this patient is unlikely due to eletriptan as it was not taken in overdose. Diazepam (175 mg), co-ingested in overdose, has a short duration of action and does not explain the prolonged coma. The delayed onset of symptoms and prolonged coma can be attributed to the delayed effect of levothyroxine (72 hours) and its long half-life, which depends upon the thyroid status of the patient. In our patient with Hashimoto’s thyroiditis, a common cause for hypothyroidism, the half-life is reported as around 10 days [6].